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Product name : GSK 1210151A (I-BET151)
Item : cc415
Price : 10mg, $275; 50mg, $845; 100mg, $1295; 200mg, $2295
contact : Send inquiry to: info@acesobio.com,or by fax to: 1-845-673-1239.
Additional Information : We offer significant discount for bulky quantity order
CAS : 
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Details:
I-BET151 (GSK1210151A) is a novel and selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4 with IC50 of ~0.5 μM, 0.25 μM, and 0.79 μM respectively. It has profound effects on human and murine MLL-fusion leukaemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action of I-BET151 is, at least in part, due to the inhibition of transcription at key genes (BCL2, C-MYC and CDK6) through the displacement of BRD3/4, PAFc and SEC components from chromatin.  In vivo studies indicate that GSK 1210151A can provide survival benefit in two distinct mouse models of murine MLL–AF9 and human MLL–AF4 leukaemia.  GSK-1210151A is also an ApoA1 upregulator that was also found to mediate potent anti-inflammatory effects. It showed a broad anti-inflammatory profile in a LPS-challenged Balb/C mouse model. [1][2]
 
Reference:
[1] Nature 2011, 478, 529-533.
[2] Bioorg. Med. Chem. Lett. 2012, 22, 2968-2972.
 
 
Chemical Information
Molecular Weight (WM):
415.44
Formula:
C23H21N5O3
CAS No:
1300031-49-5
Purity:
≥ 98%
Synonyms:
GSK1210151A
 
2 years     -20℃        Powder
Stability:
2 weeks     -4℃       in DMSO
 
2 months    -80℃       in DMSO
 
Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data.
 
PLEASE KEEP THE PRODUCT UNDER -20℃ FOR LONG-TERM STORAGE.
 
NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
 
 

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